| Reaction Details |
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 | Report a problem with these data |
| Target | MAP kinase-activated protein kinase 3 |
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| Ligand | BDBM50582077 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2153004 (CHEMBL5037551) |
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| IC50 | 1480±n/a nM |
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| Citation |  Elsner, J; Cashion, D; Robinson, D; Bahmanyar, S; Tehrani, L; Fultz, KE; Narla, RK; Peng, X; Tran, T; Apuy, J; LeBrun, L; Leftheris, K; Boylan, JF; Zhu, D; Riggs, JR Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity. J Med Chem64:12670-12679 (2021) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| MAP kinase-activated protein kinase 3 |
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| Name: | MAP kinase-activated protein kinase 3 |
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| Synonyms: | 3pK | Chromosome 3p kinase | MAP kinase-activated protein kinase 3 (MAPKAP-K3) | MAPK-Activated Protein Kinase 3 (MK3) | MAPK-activated protein kinase 3 | MAPK3_HUMAN | MAPKAP kinase 3 | MAPKAPK-3 | MAPKAPK3 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 42991.57 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant MAPKAPK3 was phosphorylated by incubation with active p38alpha before assays. |
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| Residue: | 382 |
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| Sequence: | MDGETAEEQGGPVPPPVAPGGPGLGGAPGGRREPKKYAVTDDYQLSKQVLGLGVNGKVLE
CFHRRTGQKCALKLLYDSPKARQEVDHHWQASGGPHIVCILDVYENMHHGKRCLLIIMEC
MEGGELFSRIQERGDQAFTEREAAEIMRDIGTAIQFLHSHNIAHRDVKPENLLYTSKEKD
AVLKLTDFGFAKETTQNALQTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGFP
PFYSNTGQAISPGMKRRIRLGQYGFPNPEWSEVSEDAKQLIRLLLKTDPTERLTITQFMN
HPWINQSMVVPQTPLHTARVLQEDKDHWDEVKEEMTSALATMRVDYDQVKIKDLKTSNNR
LLNKRRKKQAGSSSASQGCNNQ
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| BDBM50582077 |
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| n/a |
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| Name | BDBM50582077 |
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| Synonyms: | CHEMBL5085753 |
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| Type | Small organic molecule |
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| Emp. Form. | C42H49N9O3 |
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| Mol. Mass. | 727.897 |
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| SMILES | CCc1cccc(CC)c1N1CCn2cc(cc2C1=O)-c1nc(Nc2ccc(cc2OC)N2CCC(CC2)C(=O)N2CC3(CN(C)C3)C2)nc2[nH]ccc12 |
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| Structure | 
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